WO2012135095A3 - S1p antagonists as adjunct ocular hypotensives - Google Patents

S1p antagonists as adjunct ocular hypotensives Download PDF

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Publication number
WO2012135095A3
WO2012135095A3 PCT/US2012/030523 US2012030523W WO2012135095A3 WO 2012135095 A3 WO2012135095 A3 WO 2012135095A3 US 2012030523 W US2012030523 W US 2012030523W WO 2012135095 A3 WO2012135095 A3 WO 2012135095A3
Authority
WO
WIPO (PCT)
Prior art keywords
adjunct
antagonists
iop
ocular hypotensives
ocular
Prior art date
Application number
PCT/US2012/030523
Other languages
French (fr)
Other versions
WO2012135095A9 (en
WO2012135095A2 (en
Inventor
David F. Woodward
Todd M. Heidelbaugh
W. Daniel Stamer
Original Assignee
Allergan, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Allergan, Inc. filed Critical Allergan, Inc.
Priority to JP2014501299A priority Critical patent/JP2014508813A/en
Priority to KR1020137028029A priority patent/KR20140025412A/en
Priority to AU2012236850A priority patent/AU2012236850A1/en
Priority to CA2831290A priority patent/CA2831290A1/en
Priority to CN201280025491.4A priority patent/CN103561766A/en
Priority to RU2013147049/15A priority patent/RU2013147049A/en
Priority to BR112013024657A priority patent/BR112013024657A2/en
Priority to EP12712199.4A priority patent/EP2688593A2/en
Publication of WO2012135095A2 publication Critical patent/WO2012135095A2/en
Publication of WO2012135095A3 publication Critical patent/WO2012135095A3/en
Publication of WO2012135095A9 publication Critical patent/WO2012135095A9/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/5575—Eicosanoids, e.g. leukotrienes or prostaglandins having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/177—Receptors; Cell surface antigens; Cell surface determinants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cell Biology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention provides compositions and methods for further reducing IOP in a subject who has already achieved maximal IOP reduction using known IOP lowering agents. The activity of an ocular hypotensive treatment regimen may be increased by adding an S1P antagonist to prevent S1P mediated reversal as a result of decreased aqueous humor outflow.
PCT/US2012/030523 2011-03-25 2012-03-26 S1p antagonists as adjunct ocular hypotensives WO2012135095A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
JP2014501299A JP2014508813A (en) 2011-03-25 2012-03-26 S1P antagonist as a hypotensive aid
KR1020137028029A KR20140025412A (en) 2011-03-25 2012-03-26 S1p antagonists as adjunct ocular hypotensives
AU2012236850A AU2012236850A1 (en) 2011-03-25 2012-03-26 S1P antagonists as adjunct ocular hypotensives
CA2831290A CA2831290A1 (en) 2011-03-25 2012-03-26 S1p antagonists as adjunct ocular hypotensives
CN201280025491.4A CN103561766A (en) 2011-03-25 2012-03-26 S1P antagonists as adjunct ocular hypotensives
RU2013147049/15A RU2013147049A (en) 2011-03-25 2012-03-26 S1P ANTAGONISTS AS AUXILIARY MEANS FOR REDUCING IN-ORGAL PRESSURE
BR112013024657A BR112013024657A2 (en) 2011-03-25 2012-03-26 s1p antagonists as adjunctive ocular hypotensive
EP12712199.4A EP2688593A2 (en) 2011-03-25 2012-03-26 S1p antagonists as adjunct ocular hypotensives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161467690P 2011-03-25 2011-03-25
US61/467,690 2011-03-25

Publications (3)

Publication Number Publication Date
WO2012135095A2 WO2012135095A2 (en) 2012-10-04
WO2012135095A3 true WO2012135095A3 (en) 2013-01-17
WO2012135095A9 WO2012135095A9 (en) 2013-03-07

Family

ID=45929630

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2012/030523 WO2012135095A2 (en) 2011-03-25 2012-03-26 S1p antagonists as adjunct ocular hypotensives

Country Status (10)

Country Link
US (1) US20130079290A1 (en)
EP (1) EP2688593A2 (en)
JP (1) JP2014508813A (en)
KR (1) KR20140025412A (en)
CN (1) CN103561766A (en)
AU (1) AU2012236850A1 (en)
BR (1) BR112013024657A2 (en)
CA (1) CA2831290A1 (en)
RU (1) RU2013147049A (en)
WO (1) WO2012135095A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103740831B (en) * 2014-01-13 2015-01-28 宁波海尔施基因科技有限公司 Primer combination for guiding application of beta-receptor blocker, multi-gene detection kit and using method thereof
US20210038502A1 (en) 2017-11-08 2021-02-11 INSERM (Institut National de la Santé et de la Recherche Médicale) S1pr2 antagonists for treating diseases involving abnormal immune responses

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020103255A1 (en) * 1997-12-19 2002-08-01 Hellberg Mark R. Use of non-steroidal anti-inflammatory agents in combination with prostaglandin FP receptor agonists to treat glaucoma and ocular hypertension
US20020193441A1 (en) * 2001-02-21 2002-12-19 Robertson Stella M. Prostanoid therapies for the treatment of glaucoma
US20090004207A1 (en) * 2007-06-08 2009-01-01 Timothy Tun Hla Methods and Compositions for Inhibiting Pathological Angiogenesis in the Eye
WO2009137681A1 (en) * 2008-05-08 2009-11-12 Allergan, Inc. Therapeutically useful substituted hydropyrido [3,2,1-ij] quinoline compounds
WO2009137342A1 (en) * 2008-05-08 2009-11-12 Allergan, Inc. Therapeutically useful substituted 1, 7-diphenyl-l, 2, 3, 5, 6, 7-hexahydropyrido [ 3, 2, 1-i j ] quinoline compounds

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69328368T2 (en) * 1992-08-28 2000-08-10 Pharmos Corp., New York EMULSIONS IN THE SUBMICRON AREA AS A VEHICLE FOR DRUG ADMINISTRATION ON THE EYE

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020103255A1 (en) * 1997-12-19 2002-08-01 Hellberg Mark R. Use of non-steroidal anti-inflammatory agents in combination with prostaglandin FP receptor agonists to treat glaucoma and ocular hypertension
US20020193441A1 (en) * 2001-02-21 2002-12-19 Robertson Stella M. Prostanoid therapies for the treatment of glaucoma
US20090004207A1 (en) * 2007-06-08 2009-01-01 Timothy Tun Hla Methods and Compositions for Inhibiting Pathological Angiogenesis in the Eye
WO2009137681A1 (en) * 2008-05-08 2009-11-12 Allergan, Inc. Therapeutically useful substituted hydropyrido [3,2,1-ij] quinoline compounds
WO2009137342A1 (en) * 2008-05-08 2009-11-12 Allergan, Inc. Therapeutically useful substituted 1, 7-diphenyl-l, 2, 3, 5, 6, 7-hexahydropyrido [ 3, 2, 1-i j ] quinoline compounds

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
BOEHM A; ULRYCH T; ROSENKRANZ A C; DAUM G; GEISSLINGER G; HOHLFELD T; SCHROER K; RAUCH B H: "Release of Sphingosine-1-Phosphate From Platelets Requires Thromboxane Synthesis and Thromboxane Receptor Activation", CIRCULATION, vol. 120, no. 18, Suppl. 2, November 2009 (2009-11-01) - November 2009 (2009-11-01), 82ND SCIENTIFIC SESSION OF THE AMERICAN-HEART-ASSOCIATION; ORLANDO, FL, USA; NOVEMBER 14 -18, 2009, pages S1080, XP002680115, ISSN: 0009-7322, Retrieved from the Internet <URL:http://circ.ahajournals.org/cgi/content/meeting_abstract/120/18_MeetingAbstracts/S1080-a> [retrieved on 20120717] *
COSTAGLIOLA ET AL: "The influence of diclofenac ophthalmic solution on the intraocular pressure-lowering effect of topical 0.5% timolol and 0.005% latanoprost in primary open-angle glaucoma patients", EXPERIMENTAL EYE RESEARCH, ACADEMIC PRESS LTD, LONDON, vol. 81, no. 5, 1 November 2005 (2005-11-01), pages 610 - 615, XP005166695, ISSN: 0014-4835, DOI: 10.1016/J.EXER.2005.03.020 *
LI M H, SANCHEZ T; MILNE G L; MORROW J D; HLA T; FERRER F: "S1P/S1P2 Signaling Induces Cyclooxygenase-2 Expression in Wilms Tumor", JOURNAL OF UROLOGY, LIPPINCOTT WILLIAMS & WILKINS, BALTIMORE, MD, US, vol. 181, no. 3, 1 March 2009 (2009-03-01), pages 1347 - 1352, XP025993749, ISSN: 0022-5347, [retrieved on 20090120], DOI: 10.1016/J.JURO.2008.10.140 *
PETTUS BENJAMIN J ET AL: "The sphingosine kinase 1/sphingosine-1-phosphate pathway mediates COX-2 induction and PGE2 production in response to TNF-alpha", FASEB JOURNAL, FED. OF AMERICAN SOC. FOR EXPERIMENTAL BIOLOGY, US, vol. 17, no. 11, 1 August 2003 (2003-08-01), pages 1411 - 1421, XP002549337, ISSN: 0892-6638, DOI: 10.1096/FJ.02-1038COM *
SUMIDA G M; STAMER W D: "S1P2 receptor regulation of sphingosine-1-phosphate effects on conventional outflow physiology", AMERICAN JOURNAL OF PHYSIOLOGY - CELL PHYSIOLOGY, vol. 300, no. 5, February 2011 (2011-02-01), pages C1164 - C1171, XP002680116, DOI: DOI:10.1152/AJPCELL.00437.2010 *

Also Published As

Publication number Publication date
CA2831290A1 (en) 2012-10-04
CN103561766A (en) 2014-02-05
AU2012236850A1 (en) 2013-10-17
BR112013024657A2 (en) 2016-12-20
WO2012135095A9 (en) 2013-03-07
EP2688593A2 (en) 2014-01-29
WO2012135095A2 (en) 2012-10-04
RU2013147049A (en) 2015-04-27
KR20140025412A (en) 2014-03-04
US20130079290A1 (en) 2013-03-28
JP2014508813A (en) 2014-04-10

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